Activatable cell-penetrating peptides: a potential activatable modality for diseases diagnosis and therapy / 药学学报

Cell-penetrating peptides are composed of positively-charged amino acids that can mediate molecules or nano-carriers across cell membranes. However, most of the known cell-penetrating peptides have no cell-or tissue-specificity, with affinity to almost all types of cells in internalization. The non-specificity of cell-penetrating peptides is a significant obstacle in the application to targeted delivery of imaging probes and therapeutic agents. Accordingly, many studies focused on selective switching of systemically-delivered inert cell-penetrating peptides into active forms in diseased tissues. Tsien groups introduced the concept of activatable cell-penetrating peptides in 2004. Subsequently, a growing number of similar delivery systems (molecular or nano-sized) have been documented, and the sensitive factors have included enzyme, lower pH, light and exogenous component. In this paper, we make an overview of the development of activatable delivery system in recent years.

Research status of activatable cell-penetrating peptides-modified nanocarrier systems / 中国药学杂志

Activatable cell-penetrating peptides (ACPPs) is a new-type targeted delivery system, composed of cell-penetrating peptides, environmentally-sensitive (or stimuli-responsive) linker and shielding peptides, allowing cell-penetrating peptides high membrane permeability in specific environment or to specific stimulus, reducing systemic toxicity resulting from non-specific cellular uptake. To enhance the tumor selectivity of carriers, investigators combine ACPPs and nanocarriers in researches on cancer detection and treatment by delivering molecular probes and therapeutic agents (anticancer drugs and genes), and so on. This paper makes an overview about the reported ACPPs-modified nanocarrier systems in the recent decade.